59557-90-3Relevant academic research and scientific papers
Synthesis and anti-diabetic activity of novel biphenylsulfonamides as glucagon receptor antagonists
Lee, Chang-Yong,Choi, Hojung,Park, Eun-Young,Nguyen, Thi-Thao-Linh,Maeng, Han-Joo,Mee Lee, Kyoung,Jun, Hee-Sook,Shin, Dongyun
, p. 733 - 750 (2021/08/06)
Type 2 diabetes is characterized by chronic hyperglycemia. Insulin, a hormone secreted from pancreatic β-cells, decreases blood glucose levels, and glucagon, a hormone secreted from pancreatic α-cells, increases blood glucose levels by counterregulation of insulin through stimulation of hepatic glucose production. In diabetic patients, dysregulation of glucagon secretion contributes to hyperglycemia. Thus, inhibition of the glucagon receptor is one strategy for the treatment of hyperglycemia in type 2 diabetes. In this paper, we report a series of biphenylsulfonamide derivatives that were designed, synthesized, and then evaluated by cAMP and hepatic glucose production assays as glucagon receptor antagonists. Of these, compound 7aB-3 decreased glucagon-induced cAMP production and glucagon-induced glucose production in the in vitro assays. Glucagon challenge tests and glucose tolerance tests showed that compound 7aB-3 significantly inhibited glucagon-induced glucose increases and improved glucose tolerance. These results suggest that compound 7aB-3 has therapeutic potential for the treatment of type 2 diabetes.
An N-Fluorinated Imide for Practical Catalytic Imidations
Adachi, Akiya,Aikawa, Kohsuke,Hashimoto, Takuya,Ishibashi, Yuichiro,Oe, Yuno,Okazoe, Takashi,Tanaka, Airi,Yoshida, Ryuhei
supporting information, (2022/02/10)
Catalytic imidation using NFSI as the nitrogen source has become an emerging tool for oxidative carbon-nitrogen bond formation. However, the less than ideal benzenesulfonimide moiety is incorporated into products, severely detracting its synthetic value.
BIARYL UREA DERIVATIVE OR SALT THEREOF, AND MANUFACTURING AND APPLICATION OF SAME
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Paragraph 0135, (2019/05/10)
The present invention discloses a biaryl urea RORγt inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an RORγt inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an RORγt-related disease.
Photoactive Boron-Nitrogen-Carbon Hybrids: From Azo-borazines to Polymeric Materials
Oubaha, Hamid,Demitri, Nicola,Rault-Berthelot, Jo?lle,Dubois, Philippe,Coulembier, Olivier,Bonifazi, Davide
supporting information, p. 9101 - 9116 (2019/08/12)
In this paper, we describe synthetic routes for preparing a novel switchable BNC-based chromophore, composed of a borazine core peripherally functionalized with azobenzene moieties. Capitalizing on the Pd-catalyzed Suzuki cross-coupling reaction between a
Orthogonal switching in four-state azobenzene mixed-dimers
Zhao, Fangli,Grubert, Lutz,Hecht, Stefan,Bléger, David
supporting information, p. 3323 - 3326 (2017/03/22)
Azobenzene multi-state switches whose isomerization can be orthogonally induced with photons and electrons are presented. Exposure to green, blue, or ultraviolet light allows toggling between three isomers, while the fourth one is formed selectively via electrocatalytic isomerization.
DGAT1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0257; 0258, (2016/08/23)
The present invention discloses a novel DGAT1 inhibitor, especially the compound of formula (I) or a pharmaceutically acceptable salt thereof, preparation and pharmaceutical composition thereof, as well as their uses in the preparation of a medicament for the prevention and treatment of Familial hyperchylomicronemia (FCS), obesity, hyperlipoproteinemia or hypertriglyceridemia.
BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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Paragraph 0622; 0623; 0624, (2013/05/21)
Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.)
COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
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Page/Page column 47, (2012/02/06)
Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are
ORGANIC COMPOUNDS
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, (2011/04/14)
The present invention provides compounds of the following structure; [in-line-formulae]A-L1-B-C-D[/in-line-formulae] that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
Synthesis of arylbromides from arenes and Nbromosuccinimide bromosuccinimide (NBS) in acetonitrile - A convenient method for aromatic bromination
Zysman-Colman, Eli,Arias, Karla,Siegel, Jay S.
experimental part, p. 440 - 447 (2009/12/01)
Regioselective and chemoselective electrophilic bromination of a wide series of activated arenes using N-bromosuccinimide (NBS) in acetonitrile occurs readily. Environmentally friendly conditions, large substrate scope, and ease of synthesis enhance the utility of this method over other electrophilic bromination conditions.
